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TMPA
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TMPA图片
CAS NO:1258275-73-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
TMPA 是一种具有高亲和力的Nur77拮抗剂,与Nur77结合导致LKB1在细胞质中释放和穿梭,以激活AMPKα。TMPA 能有效地降低血糖,减轻 II 型 db/db、高脂饮食和链脲霉素诱导的糖尿病小鼠的胰岛素抵抗。TMPA 能减少人类 T 细胞的 RICD,也可用于癌症和 T 细胞凋亡失调的研究。
生物活性

TMPA is a high-affinityNur77antagonist that binds toNur77leading to the release and shuttling ofLKB1in the cytoplasm to activateAMPKα. TMPA effectively lowers blood glucose and attenuatesinsulinresistance in type II db/db, high-fat diet and streptozotocin-induced diabetic mice. TMPA reduces RICD (restimulation-induced cell death) in human T cells, can also be used in studies ofcancerand T-cellapoptosisdysregulation[1][2].

体外研究
(In Vitro)

TMPA (5, 10, 20, 40, 80 μM; 6 h or 10 μM; 0.5, 1, 3, 6, 12, 24, 36, 48 h) antagonizes the Nur77-LKB1 interaction in a dose- and time-dependent manner in hepatic LO2 cells[1].
TMPA (10 μM; 6 h) enhances the LKB1-AMPKα interaction but decreases the LKB1-Nur77 interaction under physio logical conditions in Lo2 cells[1].
TMPA binds directly to LBD in specific conformation[1].
TMPA (10, 20 μM; 6 h) induces LKB1 nuclear export to activate AMPKα in Lo2 cells[1].
TMPA (10, 50, 100 μM; 4 h) impairs human T-cell RICD (restimulation-induced cell death)[2].

Cell Viability Assay[2]

Cell Line:T cells
Concentration:10, 50, 100 μM
Incubation Time:4 h
Result:Significantly reduced T-cell RICD in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line:Hepatic LO2 cells
Concentration:10, 20 μM
Incubation Time:6 h
Result:Led to an increase of LKB1 phosphorylation at Ser428.

Western Blot Analysis[1]

Cell Line:Hepatic LO2 cells
Concentration:5, 10, 20, 40, 80 μM
Incubation Time:6 h
Result:Increased the amount of phosphorylation of AmPKα in a dose- and time-dependent manner.
Rescued the LKB1-AmPKα interaction by reducing the nur77-lKb1 interaction when at 10 μM.
体内研究
(In Vivo)

TMPA (50 mg/kg; i.p.; single daily for 19 days) is capable of lowering blood glucose and improving glucose tolerance in type II diabetic mice[1].

Animal Model:Male C57BL/KsJ-Leprdb/Leprdb(db/db) mice (10-week-old; type II diabetic model)[1].
Dosage:50 mg/kg
Administration:Intraperitoneal injection; single daily for 19 days.
Result:Significantly reduced blood glucose at day 7 and persisted during the remainder of the test.
Increased the amount of phosphorylated AMPKα in the liver of mice.
分子量

380.48

性状

Solid

Formula

C21H32O6

CAS 号

1258275-73-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL(262.83 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.6283 mL13.1413 mL26.2826 mL
5 mM0.5257 mL2.6283 mL5.2565 mL
10 mM0.2628 mL1.3141 mL2.6283 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.57 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (6.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.57 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。